Biochem/physiol Actions

Reversible: no

Target IC₅₀: 50-100 nM against chymotrypsin-like activity of the 20S proteasome

Product does not compete with ATP.

Cell permeable: yes

Primary Targetchymotrypsin-like activity of the 20S proteasome

General description

A cell-permeable, peptide vinyl sulfone that acts as a potent, irreversible inhibitor of proteasome activity. Covalently modifies the catalytically active β-subunits of the proteasome. Shown to inhibit the chymotrypsin-like (10-50 nM), trypsin-like (1-5 µM), and the peptidyl glutamyl peptide hydrolyzing (PGPH) (0.5-1 µM) activities of purified 20S proteasomes from rabbit muscle. Inhibits proteasomal degradation of deglycosylated MHC HLA-A2 heavy chain in US11+ cells (~50 µM).

A potent, covalent, cell-permeable, irreversible inhibitor of chymotrypsin-like (50-100 nM), trypsin-like (1-5 µM), and PGPH (0.5-1 µM) activities of the 20S proteasome.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Kessler, B.M., et al. 2001. Chem. Biol.8, 913.

Packaging

Packaged under inert gas

250 µg in Plastic ampoule

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)